Classifications

• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
  • A61Q11/00—Preparations for care of the teeth, of the oral cavity or of dentures; Dentifrices, e.g. toothpastes; Mouth rinses
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
  • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
  • A61K8/34—Alcohols
  • A61K8/347—Phenols
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
  • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
  • A61K8/34—Alcohols
  • A61K8/345—Alcohols containing more than one hydroxy group
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
  • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
  • A61K8/36—Carboxylic acids; Salts or anhydrides thereof
  • A61K8/368—Carboxylic acids; Salts or anhydrides thereof with carboxyl groups directly bound to carbon atoms of aromatic rings
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
  • A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
  • A61K8/44—Aminocarboxylic acids or derivatives thereof, e.g. aminocarboxylic acids containing sulfur; Salts; Esters or N-acylated derivatives thereof
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
  • A61K8/81—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds obtained by reactions involving only carbon-to-carbon unsaturated bonds
  • A61K8/8105—Compositions of homopolymers or copolymers of unsaturated aliphatic hydrocarbons having only one carbon-to-carbon double bond; Compositions of derivatives of such polymers
  • A61K8/8111—Homopolymers or copolymers of aliphatic olefines, e.g. polyethylene, polyisobutene; Compositions of derivatives of such polymers
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
  • A61K8/81—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds obtained by reactions involving only carbon-to-carbon unsaturated bonds
  • A61K8/8129—Compositions of homopolymers or copolymers of compounds having one or more unsaturated aliphatic radicals, each having only one carbon-to-carbon double bond, and at least one being terminated by an alcohol, ether, aldehydo, ketonic, acetal or ketal radical; Compositions of hydrolysed polymers or esters of unsaturated alcohols with saturated carboxylic acids; Compositions of derivatives of such polymers, e.g. polyvinylmethylether
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
  • A61K2800/20—Chemical, physico-chemical or functional or structural properties of the composition as a whole
  • A61K2800/30—Characterized by the absence of a particular group of ingredients
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
  • A61K2800/80—Process related aspects concerning the preparation of the cosmetic composition or the storage or application thereof
  • A61K2800/92—Oral administration

Definitions

• Preservative systems play a critical role in oral care formulation development. While many preservatives are able to provide the necessary anti -microbial effect, many preservatives can have undesirable effects and can also impact the flavor profile of a composition. Thus, formulators are presented with the challenge of identifying safe preservative systems which provide an acceptable level of preservation without adversely impacting the flavor profile or stability of the composition.
• Embodiments of the present invention are designed to address these, and other, needs.
• the present invention provides an oral care composition
• an orally acceptable carrier comprising greater than about 50 wt.% water
• a preservative system comprising: benzyl alcohol, benzoic acid or a salt of benzoic acid; and an alkylene glycol.
• Some embodiments further comprise a basic amino acid in free or salt form.
• the preservative system is substantially free of isothiazolinones.
• compositions described herein for: treating, preventing, reducing the incidence of, or inhibiting dental erosion; treating, preventing, reducing the incidence of, or inhibiting the formation of dental caries; occluding a dentinal tubule; treating, preventing, reducing the incidence of, or inhibiting hypersensitivity of the teeth; fostering growth of beneficial bacteria in the oral cavity; reducing, repairing or inhibiting early enamel lesions, e.g., as detected by quantitative light-induced fluorescence (QLF) or electrical caries measurement (ECM); reducing or inhibiting demineralization and promoting remineralization of the teeth; treating, preventing, reducing the incidence of, or inhibiting gingivitis; promoting healing of sores or cuts in the mouth; reducing levels of acid producing bacteria; increasing relative levels of arginolytic bacteria; inhibiting microbial bio film formation in the oral cavity; raising and/or maintaining plaque pH at levels of at least pH 5.5 following sugar challenge; reducing
• QLF quantitative light-induced fluorescence
• ECM
• Composition 1 further comprising an amino acid selected from lysine, glycine and arginine, in free or orally acceptable acid addition salt form, e.g., hydrochloride form.
• compositions wherein amino acid is present in an amount of 0.05 to 10 wt.%, e.g., about 1-5 wt.%, optionally 0.1 wt.%, 0.2 wt.%, 0.3 wt.%, 0.4 wt.%, 0.5 wt.%, 0.8 wt.%, 1 wt.%, 2 wt.%, 3 wt.%, 4 wt.%, 5 wt.%.
• compositions further comprising an effective amount of a fluoride ion source, e.g., providing 50 to 3000 ppm fluoride, e.g. from about 100 to about 500 ppm, e.g., from about 200 to about 300 ppm e.g. about 225 ppm.
• a fluoride ion source e.g., providing 50 to 3000 ppm fluoride, e.g. from about 100 to about 500 ppm, e.g., from about 200 to about 300 ppm e.g. about 225 ppm.
• compositions comprising a humectant, e.g., selected from glycerin, sorbitol, propylene glycol, polyethylene glycol, xylitol, and mixtures thereof.
• a humectant e.g., selected from glycerin, sorbitol, propylene glycol, polyethylene glycol, xylitol, and mixtures thereof.
• compositions comprising one or more surfactants, e.g., selected from anionic, cationic, zwitterionic, and nonionic surfactants, and mixtures thereof, e.g., comprising an anionic surfactant, e.g., a surfactant selected from sodium lauryl sulfate, sodium ether lauryl sulfate, and mixtures thereof, e.g. in an amount of from about 0.3% to about 4.5% by weight, e.g. 1-2% sodium lauryl sulfate (SLS); and/or a zwitterionic surfactant, for example a betaine surfactant, for example cocamidopropylbetaine, e.g. in an amount of from about 0.1% to about 4.5% by weight, e.g. 0.5-2% cocamidopropylbetaine.
• anionic surfactant e.g., a surfactant selected from sodium lauryl sulfate, sodium ether lauryl sul
• compositions further comprising polyoxyethylene.
• compositions further comprising a viscosity modifying amount of one or more of polysaccharide gums, for example xanthan gum or carrageenan, and combinations thereof. 1.14. Any of the preceding compositions further comprising flavoring, fragrance and/or coloring.
• compositions further comprising a whitening agent, e.g., a selected from the group consisting of peroxides, metal chlorites, perborates, percarbonates, peroxy acids, and combinations thereof.
• a whitening agent e.g., a selected from the group consisting of peroxides, metal chlorites, perborates, percarbonates, peroxy acids, and combinations thereof.
• Embodiments of the present invention further provide methods to reduce and inhibit acid erosion of the enamel, clean the teeth, reduce bacterially-generated biofilm and plaque, reduce gingivitis, inhibit tooth decay and formation of cavities, and reduce dentinal hypersensitivity, comprising applying an effective amount of a composition of the invention, e.g., any of Composition 1, etseq. to the teeth.
• a composition of the invention e.g., any of Composition 1, etseq.
• inventions comprise an orally acceptable base comprising ingredients selected from one or more of buffering agents, humectants, surfactants, thickeners, breath fresheners, flavoring, fragrance, coloring, antibacterial agents, whitening agents, agents that interfere with or prevent bacterial attachment, phosphate sources, orally acceptable potassium salts, and anionic polymers.
• zinc is present in an amount of 0.01 to 10% by weight of the composition.
• the amount of zinc is at least 0.1, at least 0.2, at least 0.3, at least 0.4, at least 0.5, at least 1, at least 2, at least 3, or at least 4 up to 10% by weight of the composition.
• the amount of the zinc is less than 9, less than 8, less than 7, less than 6, less than 5, less than 4, less than 3, less than 2, less than 1, less than 0.5 to 0.05 % by weight of the composition.
• the amounts are 0.05 to 5%, 0.05 to 4%, 0.05 to 3%, 0.05 to 2%, 0.1 to 5%, 0.1 to 4%, 0.1 to 3%, 0.1 to 2%, 0.5 to 5%, 0.5 to 4%, 0.5 to 3%, or 0.5 to 2% by weight of the composition.
• the total amount of zinc in the composition is 0.05 to 8 % by weight of the composition. In other embodiments, the total amount of zinc is at least 0.1, at least 0.2, at least 0.3, at least 0.4, at least 0.5, or at least 1 up to 8% by weight of the composition. In other embodiments, the total amount of zinc in the composition is less than 5, less than 4, less than 3, less than 2, or less than 1 to 0.05% by weight of the composition.
• the basic amino acid is arginine, for example, 1-arginine, or a salt thereof.
• Arginine when present, may be present at levels from, e.g., about 0.1 wt.% to about 20 wt.% (expressed as weight of free base). In some embodiments, arginine is present in an amount of from about 0.1 wt.% to about 10 wt.%, or about 0.25 wt.% to about 8 wt.%, or about 0.5 wt.% to about 4 wt.%, or about 0.75 wt.% to about 1 wt.%, or about 0.8 wt.%.
• water-soluble salts of higher fatty acid monoglyceride monosulfates such as the sodium salt of the monosulfated monoglyceride of hydrogenated coconut oil fatty acids such as sodium N-methyl N-cocoyl taurate, sodium cocomonoglyceride sulfate,
• the anionic surfactant is present in a toothpaste at from about 0.3% to about 4.5% by weight, e.g., about 1.5%.
• the compositions of the invention may optionally contain mixtures of surfactants, e.g., comprising anionic surfactants and other surfactants that may be anionic, cationic, zwitterionic or nonionic.
• surfactants are those which are reasonably stable throughout a wide pH range. Surfactants are described more fully, for example, in U.S. Pat. No. 3,959,458, to Agricola et al.; U.S. Pat. No. 3,937,807, to Haefele; and U.S. Pat. No. 4,051,234, to Gieske et al.
• Phosphate as used herein encompasses orally acceptable mono- and polyphosphates, for example, P 1-6 phosphates, for example monomeric phosphates such as monobasic, dibasic or tribasic phosphate; dimeric phosphates such as pyrophosphates; and multimeric phosphates, e.g., sodium hexametaphosphate.
• Flavorins Asents The oral care compositions of the invention may also include a flavoring agent.
• Flavoring agents which are used in the practice of the present invention include, but are not limited to, essential oils as well as various flavoring aldehydes, esters, alcohols, and similar materials.
• the essential oils include oils of spearmint, peppermint, wintergreen, sassafras, clove, sage, eucalyptus, maijoram, cinnamon, lemon, lime, grapefruit, and orange. Also useful are such chemicals as menthol, carvone, and anethole. Certain embodiments employ the oils of peppermint and spearmint.
• the flavoring agent may be incorporated in the oral composition at a concentration of about 0.01 to about 5% by weight, e.g. about 0.05 to about 1.5%, e.g. about 0.1 to about 1%, by weight.
• the oral care compositions of the invention may also include polymers to adjust the viscosity of the formulation or enhance the solubility of other ingredients.
• additional polymers include polyethylene glycols, polysaccharides (e.g., cellulose derivatives, for example caiboxymethyl cellulose, or polysaccharide gums, for example xanthan gum or carrageenan gum).
• Acidic polymers, for example polyacrylate gels may be provided in the form of their free acids or partially or fully neutralized water soluble alkali metal (e.g., potassium and sodium) or ammonium salts.
• compositions comprising from about 55 wt.% to about 70 wt.% water. While other embodiments provide compositions comprising from about 57.5 wt.% water to about 62.5 wt.% water. In some embodiments, the compositions of the present invention comprise from about 58 wt.% to about 60 wt.% water.
• compositions of the present invention and several comparative compositions which do not include the inventive preservative systems described herein.
• preservative systems can have a significant impact on the flavor profile of a composition; and finding a combination of ingredients that provides an acceptable level of preservation, as well as an acceptable flavor profile, is challenging.
• compositions 1, 8, 9 and 10 are further evaluated in a second-level flavor screening.
• the compositions are aged at 40 °C and 75% relative humidity (RH) and evaluated after eight weeks.
• RH relative humidity
• compositions 1, 8 and 10 A cosmetic evaluation is performed on the compositions that passed the flavor screen (Compositions 1, 8 and 10), and a fourth composition comprising 0.2 wt.% benzyl alcohol and 7 wt.% propylene glycol (Composition 9). Specifically, the visual appearance and color of these compositions are evaluated after four weeks at 40 °C and 49 °C. The results of these evaluations are described in Table 5 (below).

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• 2020
  • 2020-01-17 CA CA3128169A patent/CA3128169A1/en active Pending
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